(19)
(11) EP 4 424 311 A3

(12) EUROPEAN PATENT APPLICATION

(88) Date of publication A3:
18.12.2024 Bulletin 2024/51

(43) Date of publication A2:
04.09.2024 Bulletin 2024/36

(21) Application number: 24170395.8

(22) Date of filing: 17.11.2017
(51) International Patent Classification (IPC): 
C07D 487/04(2006.01)
A61K 31/519(2006.01)
A61P 35/00(2006.01)
 A61P 11/12(2006.01)
A61K 45/06(2006.01)
(52) Cooperative Patent Classification (CPC):
A61P 11/12; A61K 31/519; A61K 45/06; C07D 487/04; Y02A 50/30
(84) Designated Contracting States:
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

(30) Priority: 18.11.2016 US 201662423919 P

(62) Application number of the earlier application in accordance with Art. 76 EPC:
17872726.9 / 3541390

(71) Applicant: Cystic Fibrosis Foundation
Bethesda, MD 20814 (US)

(72) Inventors:
  • STROHBACH, Joseph Walter
    Wentzville, MO 63385 (US)
  • LIMBURG, David Christopher
    Salem, CT 06420 (US)
  • MATHIAS, John Paul
    Concord, MA 01742 (US)
  • THORARENSEN, Atli
    Stow, MA 01775 (US)
  • DENNY, Rajiah Aldrin
    Sharon, MA 02067 (US)
  • ZAPF, Christoph Wolfgang
    San Francisco, CA 94134 (US)
  • ELBAUM, Daniel
    Newman, MA 02462 (US)
  • GAVRIN, Lori Krim
    Villanova, PA 19085 (US)
  • EFREMOV, Ivan Viktorovich
    Chestnut, MA 02467 (US)

(74) Representative: J A Kemp LLP 
80 Turnmill Street
London EC1M 5QU
London EC1M 5QU (GB)

   


(54) PYRROLOPYRIMIDINES AS CFTR POTENTIATORS


(57) The present invention relates to compounds of Formula I,

wherein R1a, R1b, R2, R3, R4, W, Y, and Z are as described herein, and pharmaceutically acceptable salts thereof. The compounds are potentiators of Cystic Fibrosis Transmembrane conductance Regulator (CFTR). The invention also discloses pharmaceutical compositions comprising the compound, optionally in combination with additional therapeutic agents, and methods of potentiating, in mammals, including humans, CFTR by administration of the compounds. These compounds are useful for the treatment of cystic fibrosis (CF), asthma, bronchiectasis, chronic obstructive pulmonary disease (COPD), constipation, Diabetes mellitus, dry eye disease, pancreatitis, rhinosinusitis, Sjögren's Syndrome, and other CFTR associated disorders.





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